1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 1: discovery of the pyrrolidine scaffold and determination of its stereochemical requirements

A series of 1,3,4-trisubstituted pyrrolidines was discovered to have the ability to displace [ 125I]-MIP-1α from the CCR5 receptor expressed on Chinese hamster ovary (CHO) cell membranes. CCR5 activity was found to be dependent on the regiochemistry and the absolute stereochemistry of the pyrrolidin...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2001-06, Vol.11 (11), p.1437-1440
Main Authors: Hale, Jeffrey J., Budhu, Richard J., Mills, Sander G., MacCoss, Malcolm, Malkowitz, Lorraine, Siciliano, Salvatore, Gould, Sandra L., DeMartino, Julie A., Springer, Martin S.
Format: Article
Language:English
Subjects:
Animals
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiviral agents
Binding, Competitive
Biological and medical sciences
CCR5 Receptor Antagonists
Chemokine CCL4
CHO Cells
Cricetinae
Iodine Radioisotopes
Macrophage Inflammatory Proteins - chemistry
Macrophage Inflammatory Proteins - pharmacology
Medical sciences
Molecular Conformation
Pharmacology. Drug treatments
Pyrrolidines - chemistry
Pyrrolidines - pharmacology
Receptors, CCR5 - genetics
Transfection
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Summary:A series of 1,3,4-trisubstituted pyrrolidines was discovered to have the ability to displace [ 125I]-MIP-1α from the CCR5 receptor expressed on Chinese hamster ovary (CHO) cell membranes. CCR5 activity was found to be dependent on the regiochemistry and the absolute stereochemistry of the pyrrolidine. A series of 1,3,4-trisubstituted pyrrolidines was discovered to have the ability to displace [ 125I]-MIP-1α from the CCR5 receptor expressed on Chinese hamster ovary (CHO) cell membranes. CCR5 activity was found to be dependent on the regiochemistry and the absolute stereochemistry of the pyrrolidine.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(01)00232-3